STRUCTURAL STUDIES OF HUMAN NTP-BINDING PROTEINS

人类 NTP 结合蛋白的结构研究

• 批准号: 7954342
• 负责人: DIRKSEN E BUSSIERE
• 金额: $ 0.33万
• 依托单位: STANFORD UNIVERSITY
• 依托单位国家: 美国
• 财政年份: 2009
• 资助国家: 美国
• 起止时间: 2009-03-01 至 2010-02-28
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/7954342
• 关键词: ATP phosphohydrolase; Binding Proteins; Biological; Computer Retrieval of Information on Scientific Projects Database; Data; Drug Delivery Systems; Drug Design; Eukaryota; Funding; Generations; Goals; Grant; Human; Institution; Lead; Malignant Neoplasms; Phosphotransferases; Prokaryotic Cells; Proteins; Research; Research Personnel; Resources; Source; Structure; Synchrotrons; Therapeutic; United States National Institutes of Health; base; design; lung small cell carcinoma; malignant breast neoplasm; melanoma; programs; research study; structural biology; synchrotron radiation

This subproject is one of many research subprojects utilizing the resources provided by a Center grant funded by NIH/NCRR. The subproject and investigator (PI) may have received primary funding from another NIH source, and thus could be represented in other CRISP entries. The institution listed is for the Center, which is not necessarily the institution for the investigator. NTP-binding proteins, such as kinases and ATPases, are important effectors of biological activity in both prokaryotes and eukaryotes. Therefore, they are also important drug targets. In the following proposal we propose to perform structural studies on several key human NTP-binding proteins to further elucidate their mechanism of function, as well as to integrate these proteins into an interactive structure-based drug design cycle. Our goal is to perform structural studies on multiple projects. The structural results generated by these experiments will be used in an iterative structure-based drug design program aimed at developing therapeutics against very aggressive human cancers such as melanoma, breast cancer, and small-cell lung cancer. Rapid design and optimization of the lead compounds in such a drug design cycle is incumbent on timely access to synchrotron sources for the generation of the needed structural data.

这个子项目是许多研究子项目中利用 资源由NIH/NCRR资助的中心拨款提供。子项目和 调查员(PI)可能从NIH的另一个来源获得了主要资金， 并因此可以在其他清晰的条目中表示。列出的机构是 该中心不一定是调查人员的机构。 NTP结合蛋白，如激酶和ATPase，在原核生物和真核生物中都是重要的生物活性效应因子。因此，它们也是重要的药物靶点。在下面的提案中，我们建议对几个关键的人类NTP结合蛋白进行结构研究，以进一步阐明它们的功能机制，并将这些蛋白整合到基于结构的交互药物设计周期中。我们的目标是对多个项目进行结构研究。这些实验产生的结构结果将用于基于结构的迭代药物设计计划，旨在开发针对黑色素瘤、乳腺癌和小细胞肺癌等侵袭性极强的人类癌症的疗法。在这样的药物设计周期中，快速设计和优化先导化合物是有责任及时获得同步加速器来源，以产生所需的结构数据。